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GSK2983559
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK2983559图片

GSK2983559 (compound 3) 是一种具有口服活性且高效的受体相互作用蛋白 2 (RIP2) 激酶抑制剂。GSK2983559 在体内和人类炎症性肠病外植体样本中可阻断多种促炎细胞因子反应活性。
生物活性

GSK2983559 is an orally active and potentreceptor interacting protein 2(RIP2) kinase inhibitor. GSK2983559 blocks many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples[1].

IC50& Target[1]

RIPK2

 

体外研究
(In Vitro)

GSK2983559 (1-1024 nM; 2 h) blocks MDP-induced IL-8 in THP-1 cells[2].

Cell Viability Assay[2]

Cell Line:THP-1 cells
Concentration:1-1024 nM
Incubation Time:2 hours
Result:Inhibited IL-8 production with an IC50of 1.34 nM.
体内研究
(In Vivo)

GSK2983559 (oral gavage; 3 and 10 mg/kg; once) inhibits effectively MDP-induced IL-6 in mouse[2].

Animal Model:C57BL/6 mice (female) injected with MDP (100 μg)[2]
Dosage:3 and 10 mg/kg
Administration:Oral gavage; 3 and 10 mg/kg; once
Result:Suppressed serum IL-6 levels in a dose-dependent manner.
Clinical Trial
分子量

611.61

性状

Solid

Formula

C21H28CaN4O10PS2+

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 2 mg/mL(3.27 mM;Need ultrasonic)

DMSO :< 1 mg/mL (ultrasonic;warming;heat to 80℃)(insoluble or slightly soluble)

DMF :< 1 mg/mL (ultrasonic;warming;heat to 80℃)(insoluble)

Ethanol :< 1 mg/mL (ultrasonic)(insoluble)

*GSK2983559 is usually formulated as a suspension.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6350 mL8.1751 mL16.3503 mL
5 mM---------
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

 
 
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